邵茹辛, 吴乾虎, 李志敏, 龚雄麒. 氚标记二苯羟乙酸-3-喹宁环酯的合成J. 药学学报, 1981, 16(2): 111-113.
引用本文: 邵茹辛, 吴乾虎, 李志敏, 龚雄麒. 氚标记二苯羟乙酸-3-喹宁环酯的合成J. 药学学报, 1981, 16(2): 111-113.
Shao Ruxin, Wu Qianhu, Li Zhimin , Gong Xiongqi, . PREPARATION OF TRITIUM LABELED 3-QUINUCLIDINYL BENZILATEJ. Acta Pharmaceutica Sinica, 1981, 16(2): 111-113.
Citation: Shao Ruxin, Wu Qianhu, Li Zhimin , Gong Xiongqi, . PREPARATION OF TRITIUM LABELED 3-QUINUCLIDINYL BENZILATEJ. Acta Pharmaceutica Sinica, 1981, 16(2): 111-113.

氚标记二苯羟乙酸-3-喹宁环酯的合成

PREPARATION OF TRITIUM LABELED 3-QUINUCLIDINYL BENZILATE

  • 摘要: 本文报道了三种不同位置氚标记二苯羟乙酸喹宁环酯的制备方法。全标记产品(1)是应用一般催化氚交换法制备。苯环标记产品(Ⅱ)是先由二苯羟乙酸甲酯与氚水催化交换,然后与喹宁环醇进行酯交换而得。喹宁环3位标记产品(Ⅲ)是先以喹宁环酮催化氚化制得3(n)-3H喹宁环醇,然后再与二苯羟乙酸甲酯进行酯交换而得。其比放射性分别为6.10Ci/mmol,0.05Ci/mmol,8.76Ci/mmol。

     

    Abstract: Three tritium labeled 3-quinuclidinyl benzilates were prepared. 3-(G-3H)quinuclidinyl benzilate was prepared by a general exchange with tritiated water in the presence of platium catalyst. 3-quinuclidinyl (benzene-ZH) benzilate was prepared by catalytic tritium exchange of methyl benzilate with tritriated water, followed by ester exchange with 3-quinuclinol. 3-(3(n)-3H) quinuclidinyl benzilate was prepared by catalytic tritiation of quinuclidone, followed by ester exchange with methyl benzilate. The epecific activity were 6.10ci/mmol, O.05ci/mmol and 8.76ci/mmol respectively.

     

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